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AZD9291
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
AZD9291图片
CAS NO:1421373-65-0
规格:98%
分子量:499.61
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议
500mg电议

产品介绍

AZD9291(Osimertinib)

Mutated forms EGFR inhibitor
CAS:1421373-65-0
分子式:C28H33N7O2
分子量:499.61
纯度:98%
存储:Store at -20°C

Background:

AZD-9291 is an irreversible inhibitor of mutant EGFR kinase with IC50 values of 15nM, 17nM and 480nM, respectively for L858R/T790M, ex19del and wild-type EGFR [1].

A series of mutations cause the resistance of EGFR, AZD-9291 is developed for an irreversible and selective inhibitor of the mutant EGFR. AZD-9291 binds to the ATP binding site of EGFR by targeting Cys 797. In EGFR recombinant enzyme assay, AZD-9291 shows about 200 times greater potency against the mutant EGFR than wild-type EGFR. AZD-9291 does not exhibit significant activity towards other receptor kinase. In vitro assays show that AZD-9291can inhibit EGFR phosphorylation with lower IC50 value in cell lines harboring sensitising EGFR mutants than in wild-type cell lines. Additionally, AZD9291 can induce profound shrinkage in mutant EGFR at low doses in xenograft models. This also happens in transgenic mouse tumor models. Mice treated with AZD9291 at the dose of 5 mg/kg/day display 80% reduction in tumor volume [1].

参考文献:
[1] Darren A. E. Cross, Susan E Ashton, Serban Ghiorghiu, et al. AZD9291, an irreversible EGFR TKI, overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer. Cancer Discovery. 2014, June.